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Synthesis and Biological Evaluation of New Coumarins Bearing 2,4-Diaminothiazole-5-Carbonyl Moiety Publisher Pubmed



Ayati A1 ; Oghabi Bakhshaiesh T2 ; Moghimi S1 ; Esmaeili R2 ; Majidzadeha K2 ; Safavi M3 ; Firoozpour L1 ; Emami S4 ; Foroumadi A1, 5
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Source: European Journal of Medicinal Chemistry Published:2018


Abstract

A series of new coumarin-containing compounds 3a-l and 4a-c was designed and synthesized based on the chalcone-type 4-amino-5-cinnamoylthiazole scaffold 2, and screened for their in vitro anticancer and antioxidant activities. Representatively, the 2-thiomorpholinothiazole derivative 3k with IC50 values of 7.5–16.9 μg/ml demonstrated good cytotoxic effects against tested cell lines MCF-7, HepG2 and SW480. Further investigation by flow cytometric analysis confirmed that this compound induces apoptotic cell death in MCF-7 cells and cause G1-phase arrest in the cell cycle. Moreover, most of compounds had intrinsic potential for radical scavenging activity and ferric-reducing power as investigated by DPPH and FRAP assays. © 2018 Elsevier Masson SAS
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